Journal
MOLECULES
Volume 27, Issue 18, Pages -Publisher
MDPI
DOI: 10.3390/molecules27185781
Keywords
isatin; indole; imidazo[2; 1-b]thiazole; antimicrobial agents; cytotoxicity
Funding
- University of Bologna (RFO funds)
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Isatin and its derivatives are important heterocycles with various biological activities and are essential building blocks in organic synthesis. In this study, a small library of 18 isatin hybrids were synthesized and evaluated for antimicrobial potential, with two lead compounds showing inhibitory activity against S. aureus at very low concentrations.
Isatin and its derivatives are important heterocycles found in nature and present in numerous bioactive compounds which possess various biological activities. Moreover, it is an essential building block in organic synthesis. The discovery of novel compounds active against human pathogenic bacteria and fungi is an urgent need, and the isatin may represent the suitable scaffold in the design of biologically relevant antimicrobials. A small library of 18 isatin hybrids was synthetized and evaluated for their antimicrobial potential on three reference strains: S. aureus, E. coli, both important human pathogens infamous for causing community- and hospital-acquired severe systemic infections; and C. albicans, responsible for devastating invasive infections, mainly in immunocompromised individuals. The study highlighted two lead compounds, 6k and 6m, endowed with inhibitory activity against S. aureus at very low concentrations (39.12 and 24.83 mu g/mL, respectively).
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